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DRUG:

BMS-986299

i
Other names: BMS-986299, BMS986299, BMS 986299
Associations
Company:
BMS
Drug class:
NLRP3 agonist
Associations
1year
Phase I study of BMS-986299, an NLRP3 agonist, as monotherapy and in combination with nivolumab and ipilimumab in patients with advanced solid tumors. (PubMed, J Immunother Cancer)
BMS-986299 in combination with immune checkpoint inhibitors demonstrated manageable toxicities, good tolerability, and promising antitumor activity in certain cancer types.
P1 data • Journal
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HER-2 (Human epidermal growth factor receptor 2) • IL6 (Interleukin 6) • CD4 (CD4 Molecule) • IL1B (Interleukin 1, beta) • NLRP3 (NLR Family Pyrin Domain Containing 3)
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HR positive • HER-2 negative • EGFR positive
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Opdivo (nivolumab) • Yervoy (ipilimumab) • BMS-986299
over1year
Structural Insight into the Binding Pattern and Interaction Mechanism of Antagonist MCC950 and Agonist BMS986299 with NLRP3 by Molecular Dynamics Simulation. (PubMed, Curr Comput Aided Drug Des)
The antagonist may interact with residues mainly in the NBD, HD1, WHD, and HD2 domains, and the agonist may interact in the NBD and WHD domains. Our study provided new insights into the development of NLRP3 regulators.
Journal
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NLRP3 (NLR Family Pyrin Domain Containing 3)
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BMS-986299
almost2years
TRIM6 Promotes ROS-Mediated Inflammasome Activation and Pyroptosis in Renal Tubular Epithelial Cells via Ubiquitination and Degradation of GPX3 Protein. (PubMed, Front Biosci (Landmark Ed))
TRIM6 increases oxidative stress and promotes the pyroptosis of HK2 cells by regulating GPX3 ubiquitination. These findings could contribute to the development of novel drugs for the treatment of RF.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL18 (Interleukin 18) • IL1B (Interleukin 1, beta) • NLRP3 (NLR Family Pyrin Domain Containing 3) • GPX3 (Glutathione Peroxidase 3) • TRIM6 (Tripartite Motif Containing 6) • CASP1 (Caspase 1)
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IL6 expression
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BMS-986299
over4years
Phase 0 Master Protocol for CIVO Intratumoral Microdosing of Anti-Cancer Therapies (clinicaltrials.gov)
P1, N=36, Recruiting, Presage Biosciences | Not yet recruiting --> Recruiting | N=12 --> 36 | Initiation date: Feb 2021 --> Jun 2021
Clinical • Enrollment open • Enrollment change • Trial initiation date
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CD8 (cluster of differentiation 8) • TNFA (Tumor Necrosis Factor-Alpha) • CD163 (CD163 Molecule) • CD4 (CD4 Molecule) • NCAM1 (Neural cell adhesion molecule 1) • CASP3 (Caspase 3) • CD68 (CD68 Molecule) • GZMB (Granzyme B) • CD86 (CD86 Molecule)
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Keytruda (pembrolizumab) • Opdivo (nivolumab) • Yervoy (ipilimumab) • carboplatin • paclitaxel • 5-fluorouracil • relatlimab (BMS-986016) • BMS-986299 • MK-0482 • MK-4830 • dazostinag (TAK-676)
almost5years
[VIRTUAL] Discovery and preclinical characterization of BMS-986299, a first-in-class NLRP3 agonist with potent antitumor activity in combination with checkpoint blockade (ACS-Sp 2021)
In vivo studies demonstrated that BMS-986299 enhanced the antitumor activity of CPIs and induced durable immunological memory in solid tumor models. BMS-986299 is currently in Phase I clinical trials for the treatment of cancer.
Preclinical • Combination therapy • Checkpoint inhibition
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IL18 (Interleukin 18) • IL1B (Interleukin 1, beta)
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BMS-986299
5years
Phase 0 Master Protocol for CIVO Intratumoral Microdosing of Anti-Cancer Therapies (clinicaltrials.gov)
P1, N=12, Not yet recruiting, Presage Biosciences | Trial completion date: Dec 2030 --> Dec 2031 | Initiation date: Nov 2020 --> Feb 2021 | Trial primary completion date: Dec 2030 --> Dec 2031
Clinical • Trial completion date • Trial initiation date • Trial primary completion date
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CD8 (cluster of differentiation 8) • TNFA (Tumor Necrosis Factor-Alpha) • CD163 (CD163 Molecule) • CD4 (CD4 Molecule) • NCAM1 (Neural cell adhesion molecule 1) • CASP3 (Caspase 3) • CD68 (CD68 Molecule) • GZMB (Granzyme B) • CD86 (CD86 Molecule)
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Keytruda (pembrolizumab) • Opdivo (nivolumab) • Yervoy (ipilimumab) • carboplatin • paclitaxel • 5-fluorouracil • relatlimab (BMS-986016) • BMS-986299 • MK-0482 • MK-4830 • dazostinag (TAK-676)
over5years
Clinical • New P1 trial • PD(L)-1 Biomarker
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CD8 (cluster of differentiation 8) • TNFA (Tumor Necrosis Factor-Alpha) • CD163 (CD163 Molecule) • CD4 (CD4 Molecule) • NCAM1 (Neural cell adhesion molecule 1) • CASP3 (Caspase 3) • CD68 (CD68 Molecule) • GZMB (Granzyme B) • CD86 (CD86 Molecule)
|
Keytruda (pembrolizumab) • Opdivo (nivolumab) • Yervoy (ipilimumab) • carboplatin • paclitaxel • 5-fluorouracil • relatlimab (BMS-986016) • BMS-986299 • MK-0482 • MK-4830 • dazostinag (TAK-676)